TY - JOUR T1 - Contrasting sirtuin and poly(ADP-ribose)polymerase activities of selected 2,4,6-trisubstituted benzimidazoles. AU - Yeong,Keng Yoon, AU - Tan,Soo Choon, AU - Mai,Chun-Wai, AU - Leong,Chee-Onn, AU - Chung,Felicia Fei-Lei, AU - Lee,Yean Kee, AU - Chee,Chin Fei, AU - Abdul Rahman,Noorsaadah, Y1 - 2017/08/09/ PY - 2017/04/27/received PY - 2017/06/10/revised PY - 2017/07/08/accepted PY - 2017/7/19/pubmed PY - 2019/3/21/medline PY - 2017/7/19/entrez KW - anticancer KW - benzimidazole KW - molecular docking KW - nasopharyngeal KW - poly(ADP-ribose) polymerases KW - sirtuin SP - 213 EP - 219 JF - Chemical biology & drug design JO - Chem Biol Drug Des VL - 91 IS - 1 N2 - Both sirtuin and poly(ADP-ribose)polymerase (PARP) family of enzymes utilize NAD+ as co-substrate. Inhibitors of sirtuins and PARPs are important tools in drug discovery as they are reported to be linked to multiple diseases such as cancer. New potent sirtuin inhibitors (2,4,6-trisubstituted benzimidazole) were discovered from reported PARP inhibitor scaffold. Interestingly, the synthesized compounds have contrasting sirtuin and PARP-1 inhibitory activities. We showed that modification on benzimidazoles may alter their selectivity toward sirtuin or PARP-1 enzymes. This offers an opportunity for further discovery and development of new promising sirtuin inhibitors. Molecular docking studies were carried out to aid the rationalization of these observations. Preliminary antiproliferative studies of selected compounds against nasopharyngeal cancer cells also showed relatively promising results. SN - 1747-0285 UR - https://www.unboundmedicine.com/medline/citation/28719017/Contrasting_sirtuin_and_poly_ADP_ribose_polymerase_activities_of_selected_246_trisubstituted_benzimidazoles_ L2 - https://doi.org/10.1111/cbdd.13072 DB - PRIME DP - Unbound Medicine ER -